This invention relates to certain Aloesin derivatives with natural amino acids, peptides, and amino sugars. The compounds of the present invention possess osmoprotective properties, which are suitable for topical or oral application for the treatment of topical ailments including acne, rosacea, topical wounds, dandruff, skin disfigurements, age spots, wrinkles and fine lines, excess facial oil, and veterinary problems that result from intra-cellular dehydration and concomitant onset of intra-cellular inflammation including activation/inactivation of matrix metalloproteases (MMP), tyrosinase, proteasomes, and other enzymes in mammals.